LACTAM-CONTAINING COMPOUNDS AND DERIVATIVES THEREOF AS FACTOR XA INHIBITORS
The present application describes lactam-containing compounds and derivatives thereof of Formula I: P4—P-M-M4??I or pharmaceutically acceptable salt forms thereof, wherein ring P, if present is a 5-7 membered carbocycle or heterocycle and ring M is a 5-7 membered carbocycle or heterocycle. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.
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(2017/04/28)
Structure-activity relationships of anthranilamide-based factor Xa inhibitors containing piperidinone and pyridinone P4 moieties
Introduction of the phenyl piperidinone and phenyl pyridinone P4 moieties in the anthranilamide scaffold led to potent, selective, and orally bioavailable inhibitors of factor Xa. Anthranilamide 28 displayed comparable efficacy to apixaban in the rabbit a
Corte, James R.,Fang, Tianan,Pinto, Donald J.P.,Han, Wei,Hu, Zilun,Jiang, Xiang-Jun,Li, Yun-Long,Gauuan, Jolicia F.,Hadden, Mark,Orton, Darren,Rendina, Alan R.,Luettgen, Joseph M.,Wong, Pancras C.,He, Kan,Morin, Paul E.,Chang, Chong-Hwan,Cheney, Daniel L.,Knabb, Robert M.,Wexler, Ruth R.,Lam, Patrick Y.S.
p. 2845 - 2849
(2008/12/21)
Lactam-containing compounds and derivatives thereof as factor Xa inhibitors
The present application describes lactam-containing compounds and derivatives thereof of Formula I: or pharmaceutically acceptable salt forms thereof, wherein ring P, if present is a 5-7 membered carbocycle or heterocycle and ring M is a 5-7 membered carbocycle or heterocycle. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.
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(2008/06/13)
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